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CAS号140-53-4 对氯苯乙腈 | CAS号1679-18-1 4-氯苯硼酸 | CAS号514854-13-8 6-乙基-5-碘嘧啶-2,4-二胺 | CAS号95458-40-5 3-azidopyrimethamine | CAS号186581-53-3 重氮甲烷 | CAS号55474-40-3 1-氰基-1-(对氯苯基)-2-丁酮 | CAS号100716-90-3 N-[4-ethyl-6-ch... | CAS号143947-40-4 N,N'-(5-(4-chlo... | CAS号143947-41-5 N,N'-(5-(4-chlo... | CAS号21813-35-4 2,4-Diamino-5-(... | CAS号104484-42-6 6-ethyl-5-(3-ni... | CAS号21813-35-4 2,4-Diamino-5-(... | CAS号113338-16-2 N-[2-chloro-5-(... | CAS号113494-46-5 N'-[2-chloro-5-... | CAS号113512-19-9 6-ethyl-5-(4-me... | CAS号24851-19-2 2,4-Pyrimidined... | CAS号74124-11-1 N-[4-amino-5-(4... | CAS号74124-12-2 triacetyl-pyrim...

2-(4-氯苯基)-2-氰基乙醛置于四甲基乙二胺,Sodium Hydride,Magnesium体系中,用 四氢呋喃 作为反应溶剂,化学反应 18.0H,反应生成 乙胺嘧啶
参考文献:机械化学镁介导的嘧啶与烷基溴和氯化物的 Minisci C-H 烷基化
标题:机械化学镁介导的嘧啶与烷基溴和氯化物的 Minisci C-H 烷基化
摘要:已经报道了一种通过嘧啶衍生物和烷基卤化物的机械化学镁介导的 Minisci 反应合成 4-烷基嘧啶的新方法.该反应过程底物范围广,区域选择性好,条件温和,不需要过渡金属催化剂,溶剂和惰性气体保护.该协议的实用性已通过大规模合成,机械化学产品衍生化和抗疟药物乙胺嘧啶的制备得到证明.
DOI:10.1021/acs.Orglett.1C02241

专利信息

专利号:WO-2006046949-A1
优先权日:2004-10-22
标 题 :SYNTHESIS AND ANTIMALARIAL ACTIVITY OF PYRROLO[3,2-f]QUINAZOLINE-1,3- DIAMINE DERIVATIVES
发明人：AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R
权利人:WALTER REED ARMY INST OF RES W; AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R
摘要:The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P.vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs,. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.

专利号:EP-2690438-A1
优先权日:2012-07-24
标题:Synthesis of diverse glycosylphosphatidylinositol glycans and glycolipids from toxoplasma gondii and their application as diagnostic markers and vaccines
发明人：AZZOUZ NAHID; GOETZE SEBASTIAN; SEEBERGER PETER H; SILVA DANIEL VARON; TSAI YU-HSUAN
权利人:MAX PLANCK GESELLSCHAFT
摘要:The present invention relates to the synthesis of compounds derived from glycosylphosphatidylinositol (GPI) glycolipids from Toxoplasma gondii and the resulting products obtained. These synthetic compounds are suitable for diagnosis of toxoplasmosis and for use as a vaccine against diseases caused by infection with T. gondii.

专利号:US-9802974-B2
优先权日:2012-07-24
标 题 :Synthesis of diverse glycosylphosphatidylinositol glycans from Toxoplasma gondii and their application as vaccines and diagnostics
发明人：AZZOUZ NAHID; GÖTZE SEBASTIAN; SEEBERGER PETER H; SILVA DANIEL VARON; TSAI YU-HSUAN
权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V
摘要:The present invention relates to the synthesis of GPI-related surface antigens of the parasite Toxoplasma gondii ( T. gondii ) and the resulting products obtained. These synthetic compounds are suitable for diagnosis of toxoplasmosis, as well as vaccine against toxoplasmosis, a diseases caused by infection with T. gondii.

专利号:US-6500955-B1
优先权日:2001-02-02
标 题:One pot synthesis of [2,8-Bis (trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, a mefloquine intermediate
发明人：CHAWLA HARMANDER PAL SINGH; JOHAR PERMINDER SINGH; MITTAL ALKA; MEENA RAM AVTAR; NEGI VILLENDRA SINGH
权利人:NAT INST OF PHARMACEUTICAL EDU
摘要:The present invention provides a simple single step process for the preparation of [2,8-bis(trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, comprising the step of condensing a halo-quinoline with an alpha-picolyl derivatives in the presence of a solvent, a base and a phase transfer catalyst at −10° C. to +90° C.

专利号:US-10308663-B2
优先权日:2015-06-16
标题:Inhibitors of PTP4A3 for the treatment of cancer
发明人：LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M
权利人:LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M; UNIV VIRGINIA PATENT FOUNDATION; UNIV OF PITTSBURGH —OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
摘要:The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).

专利号:US-2012100555-A1
优先权日:2009-06-29
标题 :Synthesis And Use Of Fluorophore-Tagged Antimalarials
发明人：LEAR MARTIN JAMES; TAN KEVIN SHYONG WEI
权利人:LEAR MARTIN JAMES; TAN KEVIN SHYONG WEI
摘要:This invention includes a fluorophore-tagged antimalarial represented by the following structural formula (1) or a salt thereof. This invention relates to the synthesis of fluorophore-tagged antimalarials and describes the synthesis of a fluorophore-tagged antimalarial. These fluorophore-tagged antimalarials can be used to image live cells to determine the location of the antimalarial in the cell, identify drug resistance and growth related pathways in Plasmodium isolates, identify new drug targets and chemo-sensitizers to reverse drug resistance.